温和条件下的七元杂环形成：吡唑并[3,4-b]苯并二氮杂卓的合成途径。
The Formation of Seven-Membered Heterocycles under Mild Pictet-Spengler Conditions: A Route to Pyrazolo[3,4]benzodiazepines.
机构信息
School of Chemistry, The University of Sydney , Sydney, New South Wales 2006, Australia.
出版信息
J Org Chem. 2016 Jun 3;81(11):4883-9. doi: 10.1021/acs.joc.6b00710. Epub 2016 May 13.
PMID:27159074
Abstract
Reported is a method for the synthesis of seven-membered heterocycles via a Pictet-Spengler condensation reaction under very mild conditions. High substrate scope allows for use of aldehydes using catalytic amounts of acetic acid yielding 39-90% and ketones using catalytic amounts of trifluoroacetic acid yielding 25-83%.
摘要
本文报道了一种在非常温和的条件下通过Pictet-Spengler 缩合反应合成七元杂环的方法。高底物范围允许使用催化量的乙酸的醛，产率为 39-90%，和使用催化量的三氟乙酸的酮，产率为 25-83%。
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